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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Anagliptin (formerly known as SK0403) is a novel, potent, orally bioactive, and extremely selective DPP-4 (dipeptidyl peptidase 4) inhibitor with an IC50 of 3.8 nM. It is less selective against DPP-8/9 (IC50 = 68, 60 nM). In Japan, angliptin received approval in 2012 to treat type 2 diabetes mellitus. In clinical trials, these agents not only improved glycemic control but also improved lipid metabolism. In an animal model with high cholesterol, anagliptin had a lipid-lowering effect. This finding implied that the effect was caused by hepatic lipid synthesis being downregulated. Beyond its effects on glucose reduction, anagliptin may also have positive effects on lipid metabolism.
| Targets |
DPP-4 (IC50 = 3.8 nM); DPP-9 (IC50 = 60 nM); DPP-8 (IC50 = 68 nM)
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|---|---|
| ln Vitro |
Anagliptin (SK-0403) (0-100 μM; 24 h) educes the proliferation of smooth muscle cells induced by s-DPP-4[2].
Anagliptin (100 μM; 10 min) lowers TNF-α production in cultured monocytes[2]. Anagliptin (0.001-10 μM; 24 h) significantly reduces the activity of the protein that binds to sterol regulatory elements in HepG2 cells (21% decrease)[3]. |
| ln Vivo |
Anagliptin (SK-0403) (0.3%; in diet; 16 weeks) in mice lacking apoliporotein E (apoE) decreases atherosclerotic lesions but does not raise circulating EPC counts[2].
Anagliptin (0.3%; in diet; 4 weeks) shows a lipid-lowering effect in a hyperlipidemic mice model[3]. |
| Animal Protocol |
Male apoliporotein E (apoE)-deficient mice[2]
0.3% In diet, 16 weeks |
| References |
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| Additional Infomation |
Anagliptin is an amino acid amide.
Anagliptin is under investigation for the treatment of LDL Cholesterol, Coronary Disease, Diabetes Mellitus, Glycosylated Hemoglobin, and Dipeptidyl-Peptidase 4 Inhibitors. Anagliptin is an orally available, potent, selective inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Compared to vildagliptin, anagliptin caused longer lasting inhibition of DPP-4 activity. |
| Molecular Formula |
C19H25N7O2
|
|---|---|
| Molecular Weight |
383.46
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| Exact Mass |
383.206
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| Elemental Analysis |
C, 59.51; H, 6.57; N, 25.57; O, 8.34
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| CAS # |
739366-20-2
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| Related CAS # |
Anagliptin hydrochloride;1359670-56-6
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| PubChem CID |
44513473
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| Appearance |
White to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.661
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| LogP |
-0.34
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
643
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| Defined Atom Stereocenter Count |
1
|
| SMILES |
O=C(C1=CN2C(N=C1)=CC(C)=N2)NCC(C)(NCC(N3[C@H](C#N)CCC3)=O)C
|
| InChi Key |
LDXYBEHACFJIEL-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C19H25N7O2/c1-13-7-16-21-9-14(11-26(16)24-13)18(28)22-12-19(2,3)23-10-17(27)25-6-4-5-15(25)8-20/h7,9,11,15,23H,4-6,10,12H2,1-3H3,(H,22,28)/t15-/m0/s1
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| Chemical Name |
N-[2-[[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide
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| Synonyms |
SK-0403; SK0403; SK 0403; Brand name: Suiny
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6078 mL | 13.0392 mL | 26.0783 mL | |
| 5 mM | 0.5216 mL | 2.6078 mL | 5.2157 mL | |
| 10 mM | 0.2608 mL | 1.3039 mL | 2.6078 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04810507 | Completed | Drug: Anagliptin BID Treatment |
Type 2 Diabetes | JW Pharmaceutical | November 9, 2018 | Phase 4 |
| NCT02330406 | Completed | Drug: Anagliptin Drug: Sitagliptin |
LDL Cholesterol Diabetes Mellitus |
Institute for Clinical Effectiveness, Japan |
April 2015 | Phase 4 |
| NCT01529528 | Completed | Drug: Placebo of Anagliptin Drug: Anagliptin |
Type 2 Diabetes Mellitus | JW Pharmaceutical | May 2011 | Phase 3 |
| NCT01529541 | Completed | Drug: Anagliptin Drug: Sitagliptin |
Type 2 Diabetes Mellitus | JW Pharmaceutical | May 2011 | Phase 3 |
Lipid‐lowering effects of dipeptidyl peptidase‐4 inhibitors in low‐density lipoprotein receptor‐deficient mice with anagliptin (Ana).J Diabetes Investig.2017 Mar;8(2):155-160. |
Lipid profiling by high‐performance liquid chromatography in low‐density lipoprotein receptor‐deficient mice with anagliptin (Ana).J Diabetes Investig.2017 Mar;8(2):155-160. |
Hepatic gene expression in low‐density lipoprotein receptor‐deficient mice after anagliptin (Ana) treatment. Hepatic (a) sterol regulatory element‐binding protein (SREBP)‐1c and (b) SREBP‐2 expression levels at night.Hepatic gene expression in low‐density lipoprotein receptor‐deficient mice after anagliptin (Ana) treatment. Hepatic (a) sterol regulatory element‐binding protein (SREBP)‐1c and (b) SREBP‐2 expression levels at night.J Diabetes Investig.2017 Mar;8(2):155-160. |
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